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公开(公告)号:US5672582A
公开(公告)日:1997-09-30
申请号:US322049
申请日:1994-10-12
申请人: Daniel F. Veber , S. Dale Lewis , Jules A. Shafer , Dong-Mei Feng , Ruth F. Nutt , Stephen F. Brady
发明人: Daniel F. Veber , S. Dale Lewis , Jules A. Shafer , Dong-Mei Feng , Ruth F. Nutt , Stephen F. Brady
IPC分类号: C07D211/36 , A61K31/16 , A61K31/19 , A61K31/215 , A61K31/40 , A61K31/445 , A61K38/00 , A61P7/02 , A61P43/00 , C07C237/10 , C07C271/22 , C07D207/16 , C07D211/60 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/087 , A61K38/05
CPC分类号: C07K5/0812 , C07K5/0202 , C07K5/06078 , C07K5/06191 , A61K38/00
摘要: 4-substituted cyclohexylamine derivatives which are thrombin catalytic site inhibitors and which are useful as anticoagulants. These compounds show selectivity for thrombin over other trypsin-like enzymes and have oral bioavailability. They have the formula ##STR1## for example ##STR2##
摘要翻译: 4-取代的环己胺衍生物,它们是凝血酶催化位点抑制剂,可用作抗凝剂。 这些化合物显示凝血酶比其它胰蛋白酶样酶具有选择性并具有口服生物利用度。 它们具有公式
,例如 -
公开(公告)号:US5091366A
公开(公告)日:1992-02-25
申请号:US534001
申请日:1990-06-04
摘要: Analogs of the 17-membered ring portion of ANF wherein the cysteine moiety is replaced with dipeptidyl moieties, specifically, Phe-Pro, NMP-Pro, Pro-Pro, Val-Pro, Lys-Pro, Ile-Pro, Arg-Pro, HAr-Pro, Dly-Pro, Arg-Pro, Lys-BAr, Arg-Pro, CyA-CyA, Cys-Cys, or with .alpha.-aminoheptanoic acid result in analogs of ANF having increased potencies and metabolic stability.
摘要翻译: ANF的17-元环部分的类似物,其中半胱氨酸部分被二肽基部分,特别是Phe-Pro,NMP-Pro,Pro-Pro,Val-Pro,Lys-Pro,Ile-Pro,Arg-Pro, HAr-Pro,Dly-Pro,Arg-Pro,Lys-BAr,Arg-Pro,CyA-CyA,Cys-Cys或α-氨基庚酸导致ANF的类似物具有增加的效力和代谢稳定性。
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公开(公告)号:US5374622A
公开(公告)日:1994-12-20
申请号:US10234
申请日:1993-01-28
CPC分类号: C07K14/75 , C07K5/1016
摘要: A fibrinogen receptor antagonist of the formulaAc-Cys-Asn-Pro-(L-AMF)-Gly-Asp-Cys-OHorAc-Cys-Asn-(DiMeTzl)-(L-AMF)-Gly-Asp-Cys-OH.
摘要翻译: 式Ac-Cys-Asn-Pro-(L-AMF)-Gly-Asp-Cys-OH或Ac-Cys-Asn-(DiMeTzl) - (L-AMF)-Gly-Asp-Cys的纤维蛋白原受体拮抗剂 -哦。
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公开(公告)号:US5061693A
公开(公告)日:1991-10-29
申请号:US386533
申请日:1989-07-28
申请人: Ruth F. Nutt , Stephen F. Brady , Daniel F. Veber
发明人: Ruth F. Nutt , Stephen F. Brady , Daniel F. Veber
摘要: A fibrinogen receptor antagonist compound of the structure:A--B--C--Gly--Asp--D--E (I)wherein A, B, C, D and E are preferably defined as follows:A is L-asparagine, D-asparagine or acylated asparagineB is an L-or D-isomer of proline, thioproline, .beta.,.beta.-dimethylthioproline, or N-methylalanine;C is arginine;D is phenylalanine, tryptophan .alpha.-naphthylalanine, .beta.-napthlalanine, arginine or lysine; andE is OH.
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公开(公告)号:US5023233A
公开(公告)日:1991-06-11
申请号:US386395
申请日:1989-07-28
申请人: Ruth F. Nutt , Stephen F. Brady , Daniel F. Veber
发明人: Ruth F. Nutt , Stephen F. Brady , Daniel F. Veber
摘要: A fibrinogen receptor antagonist of the formula: ##STR1## wherein A, B, C, D, E, R, R.sup.1 and X-Y are preferably defined as follows:A is acylamido;R and R.sup.1 are H;X-Y is S--S;B is L-asparagine;C is proline or thioproline or .beta., .beta.-dimethylthroprolineD is arginine; andE is COOH.
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公开(公告)号:US5338723A
公开(公告)日:1994-08-16
申请号:US948331
申请日:1992-09-21
CPC分类号: C07K14/75 , C07K5/1016
摘要: A fibrinogen receptor antagonist of the formula ##STR1## wherein XX represents a synthetic alpha-amino acid containing a linear side chain and ZZ represents a sequence of 1, 2, 3 or 4 amino acids.
摘要翻译: 一种下式的纤维蛋白原受体拮抗剂,其中XX代表含有线性侧链的合成α-氨基酸,ZZ代表1,2,3或4个氨基酸的序列。
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公开(公告)号:US5204328A
公开(公告)日:1993-04-20
申请号:US789378
申请日:1991-11-05
摘要: Atrial natriuretic factor analogs containing N-alkylated amino acids and showing enhanced potency and increased metabolic stability. These analogs have natriuretic, diuretic and vasorelaxant activity, making them suitable for treating congestive heart failure and renal hypertension.
摘要翻译: 含有N-烷基化氨基酸的心房利钠因子类似物,显示出增强的效力和增加的代谢稳定性。 这些类似物具有利钠,利尿和血管舒张活性,使其适用于治疗充血性心力衰竭和肾性高血压。
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公开(公告)号:US4816443A
公开(公告)日:1989-03-28
申请号:US51980
申请日:1987-05-19
申请人: Stephen F. Brady , Ruth F. Nutt
发明人: Stephen F. Brady , Ruth F. Nutt
IPC分类号: A61K38/00 , A61P7/10 , A61P9/00 , A61P9/12 , C07K7/08 , C07K14/00 , C07K14/575 , C07K14/58 , A61K37/02 , C07K7/10
摘要: Novel peptides having potent natriuretic activity are disclosed with the following amino acid sequence: ##STR1## wherein Z is H, acetyl, Boc or Ser-Leu, E is Phe, NMP, OMT, ChA, F is Gly or DAl, G is Ala or Gly, H is Arg or DAr, Pro, Lys or Dly, I is Ile, Met, MeO, MO.sub.2, Leu, Nle, or Val, J is Aib, .alpha.MG or .alpha.MA, K is Arg or Lys, L is Ile or Val, M is Aib, Gly, Ala or DAl, N is Ala, NMA, Pro, Phe or NMP, O is Gln, DGl, Ala or DAl, P is Ser, His, Arg or Lys, Q is Gly, Pro, Ala or Dal, R is Leu, Phe or ChA, S is Gly, Ala or Dal, Arg or DAr, T is Asn DAs, Ala or Dal, U is Ser, DSe, Ala or DAl, V is Phe, DPh, Ala or DAl, Y is -OH or -NH.sub.2 and n is 0 or 1. Also included are the lower alkyl esters and the physiologically acceptable metal salts and acid addition salts of the foregoing peptides. Unless indicated otherwise all optically active amino acids have the L-configuration.
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公开(公告)号:US4609725A
公开(公告)日:1986-09-02
申请号:US658350
申请日:1984-10-09
摘要: Monoiodinated-tyrosine derivatives of synthetic fragments of mammalian atrial natriuretic factor are biologically active and are useful to determine the mode of biological activity and the effect of derivatization on biological activity.
摘要翻译: 哺乳动物心房利钠因子合成片段的单碘化酪氨酸衍生物具有生物活性,可用于确定生物活性的模式和衍生化对生物活性的影响。
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公开(公告)号:US3963691A
公开(公告)日:1976-06-15
申请号:US512563
申请日:1974-10-07
CPC分类号: C07K5/0821 , C07K5/1005 , C07K7/23 , A61K39/00 , Y10S514/80 , Y10S530/812 , Y10S530/815 , Y10S930/13 , Y10S930/28
摘要: Synthetic antigens related to luteinizing hormone-releasing hormone (hereinafter designated LH-RH) having the amino acid composition, pyroglutamyl-histidyl-tryptophanylseryl-tyrosyl-glycyl-leucyl-arginyl-prolyl-glycyl-poly-L-lysine (hereinafter designated pyroglu-his-trp-ser-tyr-glyleu-arg-pro-gly-poly-L-lys) and poly-L-lysyl-glutarylhistidyl-tryptophanyl-seryl-tyrosyl-glycyl-leucyl-arginylprolyl-glycine amide (hereinafter designated poly-L-lysglutaryl-his-trp-ser-tyr-gly-leu-arg-pro-gly) are prepared by coupling the corresponding decapeptide with poly-L-lysine. The corresponding decapeptides are prepared by controlled stepwise procedures starting with individual amino acid components. These antigens have the property of inducing formation of antibodies to luteinizing hormone-releasing hormone (LH-RH) in animals.
摘要翻译: 与具有氨基酸组成的促黄体激素释放激素(以下称为LH-RH)相关的合成抗原,焦谷氨酰 - 组氨酰基 - 色氨酰基 - 酰基 - 酪氨酰 - 甘氨酰 - 亮氨酰 - 精氨酰 - 脯氨酰 - 甘氨酰 - 聚-L-赖氨酸(以下称为pyroglu- his-trp-ser-tyr-glyleu-arg-pro-gly-poly-L-lys)和聚-L-赖氨酰 - 戊二酰基组氨酰基 - 色氨酸 - 丝氨酰 - 酪氨酰 - 甘氨酰 - 亮氨酰 - 炔丙基 - 甘氨酰胺(下文称为聚 - 通过将相应的十肽与聚-L-赖氨酸偶联来制备L-赖氨酰赖氨基-he-trp-ser-tyr-gly-leu-arg-pro-gly)。 相应的十肽通过从各个氨基酸组分开始的受控逐步方法制备。 这些抗原具有在动物体内诱导形成促黄体激素释放激素(LH-RH)的抗体的性质。
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